Comparative Studies of Complex Products Based on Heparins of Animal and Plant Origin

M. S. Uspenskaya, L. A. Lyapina, S. M. Sorokoletov, M. G. Lyapina, M. D. Kalugina
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Abstract

Complex preparations based on heparins of animal and vegetable origin with the inclusion of glutamic acid in a weight ratio of 1 : 4 were obtained. High molecular weight (HMН) and low molecular weight (LMH) commercial preparations of heparins were used as heparins of animal origin; heparinoid was used as heparin of plant origin, isolated from the roots of the peony Akademik Sadovnichiy (heparinoid). Their influence on the state of plasma hemostasis under in vitro conditions was studied in a comparative aspect. It has been established that all complex compounds have anticoagulant activity, which, according to the results of our studies, is realized by a different mechanism of their action on blood coagulation—on the internal, external, or general pathways of blood coagulation. HMН complexes with glutamic acid had an antithrombin effect, affecting the internal and general coagulation pathways, while LMH complexes with glutamic acid, exerting anti-Xa activity, affected the internal pathway of coagulation activation, and the combination of heparinoid with glutamic acid inhibited factors of not only internal but also external ways of blood coagulation. In addition, the latter compound exhibited weak antithrombin activity. It was also shown that all heparin complexes prevented fibrin polymerization, increasing the fibrin depolymerization activity of plasma, and in the heparinoid compound, this activity was higher by 10–17% compared to other commercial agents. Thus, the best anticoagulant in terms of efficacy and safety is the heparinoid complex with glutamic acid.

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动植物源性肝素复合产品的比较研究
摘要以动物源肝素和植物源肝素为原料,以1:4的质量比包合谷氨酸,制备了复方制剂。采用高分子量(HMН)和低分子量(LMH)的商业肝素制剂作为动物源性肝素;肝素为植物源肝素,从牡丹Akademik Sadovnichiy (heparinoid)根中分离得到。比较研究了它们对体外条件下血浆止血状态的影响。已经确定,所有复杂化合物都具有抗凝血活性,根据我们的研究结果,这是通过它们对血液凝固作用的不同机制实现的-在血液凝固的内部,外部或一般途径上。HMН与谷氨酸配合物具有抗凝血酶作用,影响内部和一般凝血途径,而与谷氨酸配合物具有抗xa活性,影响凝血激活的内部途径,类肝素与谷氨酸联用不仅抑制内部凝血途径,而且抑制外部凝血途径的因子。另外,后者表现出较弱的抗凝血酶活性。所有肝素复合物均能阻止纤维蛋白聚合,提高血浆纤维蛋白解聚活性,其中类肝素复合物的活性比其他市售药物高10-17%。因此,就疗效和安全性而言,最好的抗凝血剂是谷氨酸类肝素复合物。
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